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贝匹地酸:一种有前途的 LDL-C 降低新型药物。

Bempedoic acid: a promising novel agent for LDL-C lowering.

机构信息

Division of Cardiology, Washington University School of Medicine, 660 S. Euclid, Campus Box 8086, St Louis, MO 63110, USA.

Division of Endocrinology, Metabolism & Lipid Research, Washington University School of Medicine, 660 S. Euclid, Campus Box 8127, St Louis, MO 63110, USA.

出版信息

Future Cardiol. 2020 Sep;16(5):361-371. doi: 10.2217/fca-2020-0016. Epub 2020 May 28.

Abstract

Bempedoic acid (ETC-1002) is a novel, first-in-class, oral, small molecule that inhibits cholesterol biosynthesis in the same pathway as statins, thereby lowering low-density lipoprotein cholesterol (LDL-C) by upregulating LDL receptors. Preclinical and completed Phase II and III clinical trials have demonstrated promising results regarding its safety and efficacy across a variety of patient characteristics including statin intolerance and on a background of lipid-lowering therapy. Bempedoic acid is currently being evaluated in a cardiovascular outcomes trial to evaluate its effect on major cardiovascular events in patients with or at high risk for cardiovascular disease and with statin intolerance. In this review, we will discuss the history and development of bempedoic acid, relevant clinical trials, and its potential role as a lipid-lowering medication in the context of other currently available lipid-lowering therapies.

摘要

贝匹地酸(ETC-1002)是一种新型、首创的、口服、小分子药物,可通过上调 LDL 受体抑制与他汀类药物相同的胆固醇生物合成途径,从而降低 LDL 胆固醇(LDL-C)。临床前和已完成的 II 期和 III 期临床试验表明,该药在各种患者特征(包括他汀类不耐受和降脂治疗背景下)中具有良好的安全性和疗效。贝匹地酸目前正在一项心血管结局试验中进行评估,以评估其在他汀类不耐受的心血管疾病或有心血管疾病高危因素的患者中对主要心血管事件的影响。在这篇综述中,我们将讨论贝匹地酸的历史和发展、相关临床试验,以及其作为一种降脂药物在目前可用的其他降脂治疗中的潜在作用。

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